Page 79 - HIV/AIDS Guidelines

Table 6. Advantages and Disadvantages of Antiretroviral Components Recommended as
Initial Antiretroviral Therapy (page 3 of 4)

ARV
ARV Class Advantages Disadvantages
Agent(s)
PIs (in LPV/r • Coformulated • Requires 200 mg per day of RTV
alphabetical • No food requirement • Lower drug exposure in pregnant women—may need dose
order) increase in third trimester
• Recommended PI in pregnant
women (twice daily only) • Once-daily dosing not recommended in pregnant women
• Greater CD4 count increase than • Once-daily dosing results in lower trough concentration than
with EFV-based regimens twice-daily dosing
• Possible higher risk of MI associated with cumulative use of
LPV/r
• PR and QT interval prolongation have been reported. Use with
caution in patients at risk of cardiac conduction abnormalities
or receiving other drugs with similar effect.

SQV/r • Similar efficacy but less • Highest pill burden (6 pills per day) among available PI
hyperlipidemia than with LPV/r regimens
• Requires 200 mg of RTV
• Food requirement
• PR and/or QT interval prolongations in a healthy volunteer
study
• Pretreatment ECG recommended
• SQV/r is not recommended for patients with any of the
following conditions: (1) congenital or acquired QT
prolongation; (2) pretreatment ECG >450 msec; (3) on
concomitant therapy with other drugs that prolong QT
interval; (4) complete AV block without implanted
pacemakers; (5) risk of complete AV block.
INSTI RAL • Virologic response noninferior • Twice-daily dosing
to EFV • Lower genetic barrier to resistance than with boosted PI-
• Fewer drug-related adverse based regimens
events and lipid changes than • No data with NRTIs other than TDF/FTC in ART-naive patients
EFV
• Increase in creatine kinase, myopathy, and rhabdomyolysis
• No food effect have been reported
• Fewer drug-drug interactions • Rare cases of severe skin reactions (including SJS and TEN)
than PI- or NNRTI-based have been reported and systemic HSRs with rash and
regimens constitutional symptoms, with or without hepatitis, have been
reported.
CCR5 MVC • Virologic response noninferior • Requires viral tropism testing prior to initiation of therapy,
Antagonist to EFV in post hoc analysis of which results in additional cost and possible delay in initiation
MERIT study (See text.) of therapy
• Fewer adverse effects than EFV • More MVC-treated than EFV-treated patients discontinued
therapy due to lack of efficacy in MERIT study
• Less long-term experience in ART-naive patients than with
boosted PI- or NNRTI-based regimens
• Limited experience with dual-NRTIs other than ZDV/3TC
• Twice-daily dosing
• CYP 3A4 substrate; dosing depends on presence or absence of
concomitant CYP3A4 inducer(s) or inhibitor(s)

Guidelines for the Use of Antiretroviral Agents in HIV-1-Infected Adults and Adolescents F-18

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